Friday, May 25, 2012

Pharmacokinetics of Nimetazepam

 Nimetazepam

Nimetazepam (marketed under brand name Erimin) is an intermediate-acting hypnotic drug which is a benzodiazepine derivative. It was first synthesized by a team at Hoffmann-La Roche in 1962. It possesses hypnotic, anxiolytic, sedative, and skeletal muscle relaxant properties.

Taken orally, nimetazepam has very good bioavailability with nearly 100% being absorbed from the gut. It is among the most rapidly absorbed and quickest acting oral benzodiazepines, and hypnotic effects are typically felt within 15–30 minutes after oral ingestion. The blood level decline of the parent drug was biphasic with the short half-life ranging from 0.5-0.7 hours and the terminal half-life from 8–26.5 hours (mean 17.25 hours). It is the N-methylated analogue of nitrazepam (Mogadon, Alodorm), to which it is partially metabolised. Nitrazepam has a long elimination half-life, so effects of repeated dosage tend to be cumulative.

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